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First-in-Class Small Molecule to Inhibit CYP11A1 and Steroid Hormone Biosynthesis.

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|September 21, 2022
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Summary
This summary is machine-generated.

A new drug, ODM-208, effectively inhibits all steroid hormone synthesis by targeting CYP11A1. This approach shows promise for treating hormone-driven cancers like castration-resistant prostate cancer when essential steroids are replaced.

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Area of Science:

  • Endocrinology
  • Oncology
  • Drug Discovery

Background:

  • Steroid hormone receptor binding drives growth in many prostate and breast cancers.
  • CYP11A1 catalyzes the crucial initial step in all steroid hormone biosynthesis.
  • Targeting CYP11A1 offers a potential strategy to halt steroidogenesis.

Purpose of the Study:

  • To develop a selective, orally available inhibitor of CYP11A1.
  • To assess the safety and efficacy of the developed inhibitor, ODM-208.
  • To evaluate the feasibility of inhibiting steroid hormone biosynthesis in cancer patients.

Main Methods:

  • Virtual screening and structure-activity relationship optimization were employed to design ODM-208.
  • Safety and efficacy studies were conducted in animal models (rats, dogs, mice) and human patients.
  • Liquid chromatography-mass spectrometry was used to measure blood steroid hormone concentrations.

Main Results:

  • ODM-208 was identified as the first selective, nonsteroidal, oral CYP11A1 inhibitor.
  • ODM-208 demonstrated rapid, complete, durable, and reversible inhibition of steroid hormone biosynthesis in vitro and in vivo.
  • Serum steroid hormone levels became undetectable within weeks, with good tolerability when essential steroids were replaced.

Conclusions:

  • Small-molecule inhibition of CYP11A1 can effectively suppress steroid hormone biosynthesis.
  • ODM-208 is a feasible therapeutic agent for hormone-dependent cancers, particularly when combined with corticosteroid replacement therapy.
  • This strategy holds potential for managing castration-resistant prostate cancer and other steroid-driven malignancies.